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Literature for peptidase S08.039: PCSK9 peptidase

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(References are filtered for relevance to Inhibitor. To remove the filter click here. See explanation.)

    2025
  1. Koren,M.J., Vega,R.B., Agrawal,N., Xu,Y., Barbour,A.M., Yu,H., Wallerstedt,E., Carter,D., Middlemiss,J., Twaddle,L., McCarthy,M.C. and Rosenmeier,J.B.
    An Oral PCSK9 Inhibitor for Treatment of Hypercholesterolemia: The PURSUIT Randomized Trial
    J Am Coll Cardiol PubMed  Europe PubMed DOI  I
    2. 2024
  2. Agarwala,A., Asim,R. and Ballantyne,C.M.
    Oral PCSK9 Inhibitors
    Curr Atheroscler Rep26, 147-152. PubMed  Europe PubMed DOI  V  I
  3. Siddiqui,Z. and Frishman,W.
    New Oral PCSK9 Inhibitor: "MK-0616"
    Cardiol Rev PubMed  Europe PubMed DOI  K  I
  4. Wang,W.Z., Liu,C., Luo,J.Q., Lei,L.J., Chen,M.H., Zhang,Y.Y., Sheng,R., Li,Y.N., Wang,L., Jiang,X.H., Xiao,T.M., Zhang,Y.H., Li,S.W., Wu,Y.X., Xu,Y., Xu,Y.N. and Si,S.Y.
    A novel small-molecule PCSK9 inhibitor E28362 ameliorates hyperlipidemia and atherosclerosis
    Acta Pharmacol Sin45, 2119-2133. PubMed  Europe PubMed DOI  I
  5. Zhang,Q., Miao,M., Cao,S., Liu,D., Cao,Z., Bai,X., Yin,Y., Jin,S., Dong,L. and Zheng,M.
    PCSK9 promotes vascular neointimal hyperplasia through non-lipid regulation of vascular smooth muscle cell proliferation, migration, and autophagy
    Biochem Biophys Res Commun742, 151081-151081. PubMed  Europe PubMed DOI  I
    6. 2023
  6. Ballantyne,C.M., Banka,P., Mendez,G., Garcia,R., Rosenstock,J., Rodgers,A., Mendizabal,G., Mitchel,Y. and Catapano,A.L.
    Phase 2b Randomized Trial of the Oral PCSK9 Inhibitor MK-0616
    J Am Coll Cardiol81, 1553-1564. PubMed  Europe PubMed DOI  I
  7. Burnett,J.R. and Hooper,A.J.
    MK-0616: an oral PCSK9 inhibitor for hypercholesterolemia treatment
    Expert Opin Investig Drugs32, 873-878. PubMed  Europe PubMed DOI  I
  8. Iqbal,M., Hasanah,N., Arianto,A.D., Aryati,W.D., Puteri,M.U. and Saputri,F.C.
    Brazilin from Caesalpinia sappan L. as a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor: Pharmacophore-Based Virtual Screening, In Silico Molecular Docking, and In Vitro Studies
    Adv Pharmacol Pharm Sci2023, 5932315-5932315. PubMed  Europe PubMed DOI  I
  9. [YEAR:11-7-2023]Johns,D.G., Campeau,L.C., Banka,P., Bautmans,A., Bueters,T., Bianchi,E., Branca,D., Bulger,P.G., Crevecoeur,I., Ding,F.X., Garbaccio,R.M., Guetschow,E.D., Guo,Y., Ha,S.N., Johnston,J.M., Josien,H., Kauh,E.A., Koeplinger,K.A., Kuethe,J.T., Lai,E., Lanning,C.L., Lee,A.Y.H., Li,L., Nair,A.G., O'Neill,E.A., Stoch,S.A., Thaisrivongs,D.A., Tucker,T.J., Vachal,P., van,D.K., Vanhoutte,F.P., Volckaert,B., Wolford,D.G., Xu,A., Zhao,T., Zhou,D., Zhou,S., Zhu,X., Zokian,H.J., Walji,A.M. and Wood,H.B.
    Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor
    Circulation148, 144-158. PubMed  Europe PubMed  I
  10. Kuethe,J.T., Lee,J., Thaisrivongs,D., Yasuda,N., Pollack,S.R., Leone,J., DaSilva,J., Biba,M., Tsay,F.R., Regalado,E.L., Qi,J., Li,H., Poggetto,G.D. and Cohen,R.
    Synthesis of a Complex and Highly Potent PCSK9 Inhibitor
    Org Lett25, 5001-5005. PubMed  Europe PubMed DOI  I
    11. 2021
  11. Masagalli,J.N., BasavanaGowda,M.K., Chae,H.S. and Choi,W.J.
    Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells
    Molecules26, DOI  I
  12. Masagalli,J.N., BasavanaGowda,M.K., Chae,H.S. and Choi,W.J.
    Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells
    Molecules26, PubMed  Europe PubMed DOI  I
    13. 2020
  13. Adorni,M.P., Zimetti,F., Lupo,M.G., Ruscica,M. and Ferri,N.
    Naturally occurring PCSK9 inhibitors
    Nutrients12, PubMed  Europe PubMed DOI  I
  14. Evison,B.J., Palmer,J.T., Lambert,G., Treutlein,H., Zeng,J., Nativel,B., Chemello,K., Zhu,Q., Wang,J., Teng,Y., Tang,W., Xu,Y., Rathi,A.K., Kumar,S., Suchowerska,A.K., Parmar,J., Dixon,I., Kelly,G.E. and Bonnar,J.
    A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove
    Bioorg Med Chem28, 115344-115344. PubMed  Europe PubMed DOI  I
  15. Petrilli,W.L., Adam,G.C., Erdmann,R.S., Abeywickrema,P., Agnani,V., Ai,X., Baysarowich,J., Byrne,N., Caldwell,J.P., Chang,W., DiNunzio,E., Feng,Z., Ford,R., Ha,S., Huang,Y., Hubbard,B., Johnston,J.M., Kavana,M., Lisnock,J.M., Liang,R., Lu,J., Lu,Z., Meng,J., Orth,P., Palyha,O., Parthasarathy,G., Salowe,S.P., Sharma,S., Shipman,J., Soisson,S.M., Strack,A.M., Youm,H., Zhao,K., Zink,D.L., Zokian,H., Addona,G.H., Akinsanya,K., Tata,J.R., Xiong,Y. and Imbriglio,J.E.
    From screening to targeted degradation: strategies for the discovery and optimization of small molecule ligands for PCSK9
    Cell Chem Biol27, 32-40. PubMed  Europe PubMed DOI  S  I
  16. Shingai,Y., Kimura,N., Doijiri,R., Takahashi,K., Yokosawa,M., Kanoke,A., Kikuchi,T., Sugawara,T. and Tominaga,T.
    Effect of preoperative administration of proprotein convertase subtilisin/kexin type 9 inhibitor on carotid artery stenting
    World Neurosurg135, e36-e36. PubMed  Europe PubMed DOI  I
    17. 2019
  17. Ferrari,F., Stein,R., Motta,M.T. and Moriguchi,E.H.
    PCSK9 Inhibitors: clinical relevance, molecular mechanisms, and safety in clinical practice
    Arq Bras Cardiol112, 453-460. PubMed  Europe PubMed DOI  I
  18. Guarnieri,F., Kulp JL Jr, Kulp JL 3rd and Cloudsdale,I.S.
    Fragment-based design of small molecule PCSK9 inhibitors using simulated annealing of chemical potential simulations
    PLoS ONE14, e0225780-e0225780. PubMed  Europe PubMed DOI  I
  19. Lammi,C., Sgrignani,J., Arnoldi,A., Lesma,G., Spatti,C., Silvani,A. and Grazioso,G.
    Computationally driven structure optimization, synthesis, and biological evaluation of imidazole-based proprotein convertase subtilisin/kexin 9 (PCSK9) inhibitors
    J Med Chem62, 6163-6174. PubMed  Europe PubMed DOI  I
  20. Lammi,C., Sgrignani,J., Arnoldi,A. and Grazioso,G.
    Biological characterization of computationally designed analogs of peptide TVFTSWEEYLDWV (Pep2-8) with increased PCSK9 antagonistic activity
    Sci Rep9, 2343-2343. PubMed  Europe PubMed DOI  I
  21. Palee,S., McSweeney,C.M., Maneechote,C., Moisescu,D.M., Jaiwongkam,T., Kerdphoo,S., Chattipakorn,S.C. and Chattipakorn,N.
    PCSK9 inhibitor improves cardiac function and reduces infarct size in rats with ischaemia/reperfusion injury: benefits beyond lipid-lowering effects
    J Cell Mol Med23, 7310-7319. PubMed  Europe PubMed DOI  I
    22. 2018
  22. Nishikido,T. and Ray,K.K.
    Non-antibody approaches to proprotein convertase subtilisin kexin 9 inhibition: siRNA, antisense oligonucleotides, adnectins, vaccination, and new attempts at small-molecule inhibitors based on new discoveries
    Front Cardiovasc Med5, 199-199. PubMed  Europe PubMed DOI  I
  23. Pettersen,D. and Fjellstrom,O.
    Small molecule modulators of PCSK9 - a literature and patent overview
    Bioorg Med Chem Lett28, 1155-1160. PubMed  Europe PubMed DOI  V  I
    24. 2017
  24. Zhang,Y., Ultsch,M., Skelton,N.J., Burdick,D.J., Beresini,M.H., Li,W., Kong-Beltran,M., Peterson,A., Quinn,J., Chiu,C., Wu,Y., Shia,S., Moran,P., Di Lello,P., Eigenbrot,C. and Kirchhofer,D.
    Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists
    Nat Struct Mol Biol24, 848-856. PubMed  Europe PubMed DOI  I
    25. 2016
  25. Salowe,S.P., Zhang,L., Zokian,H.J., Gesell,J.J., Zink,D.L., Wiltsie,J., Ai,X., Kavana,M. and Pinto,S.
    In vitro assays for the discovery of PCSK9 autoprocessing inhibitors
    J Biomol Screen21, 1034-1041. PubMed  Europe PubMed DOI  I
    26. 2015
  26. Dragan,S., Serban,M.C. and Banach,M.
    Proprotein convertase subtilisin/kexin 9 inhibitors: an emerging lipid-lowering therapy?
    J Cardiovasc Pharmacol Ther20, 157-168. PubMed  Europe PubMed DOI  I
  27. EBioMedicine
    PCSK9 inhibitors: what lies beyond monoclonal antibodies?
    EBioMedicine2, 1835-1835. PubMed  Europe PubMed DOI  I
  28. Pokharel,Y., Virani,S.S. and Ballantyne,C.M.
    The promise of proprotein convertase subtilisin/kexin 9 inhibitors for the treatment of familial hypercholesterolemia
    Curr Atheroscler Rep17, 508-508. PubMed  Europe PubMed DOI  I
    29. 2014
  29. Chorba,J.S. and Shokat,K.M.
    The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis
    J Biol Chem289, 29030-29043. PubMed  Europe PubMed DOI  M  I
  30. Zhang,Y., Eigenbrot,C., Zhou,L., Shia,S., Li,W., Quan,C., Tom,J., Moran,P., Di Lello,P., Skelton,N.J., Kong-Beltran,M., Peterson,A. and Kirchhofer,D.
    Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor
    J Biol Chem289, 942-955. PubMed  Europe PubMed DOI  S  I
    31. 2013
  31. Do,R.Q., Vogel,R.A. and Schwartz,G.G.
    PCSK9 inhibitors: potential in cardiovascular therapeutics
    Curr Cardiol Rep15, 345-345. PubMed  Europe PubMed DOI  T  I
  32. Farnier,M.
    PCSK9 inhibitors
    Curr Opin Lipidol24, 251-258. PubMed  Europe PubMed DOI  I
  33. Hooper,A.J. and Burnett,J.R.
    Anti-PCSK9 therapies for the treatment of hypercholesterolemia
    Expert Opin Biol Ther13, 429-435. PubMed  Europe PubMed DOI  I
  34. Lee,P. and Hegele,R.A.
    Current phase II proprotein convertase subtilisin/kexin 9 inhibitor therapies for dyslipidemia
    Expert Opin Investig Drugs22, 1411-1423. PubMed  Europe PubMed DOI  I
  35. Li,C.Y., Bai,Y. and Qin,Y.W.
    Research advances in proprotein convertase subtilisin/kexin type 9 inhibitors
    Pharm Care Res13, 241-244. DOI  I
  36. Shen,L., Peng,H., Xu,D. and Zhao,S.
    The next generation of novel low-density lipoprotein cholesterol-lowering agents: proprotein convertase subtilisin/kexin 9 inhibitors
    Pharmacol Res73, 27-34. PubMed  Europe PubMed DOI  I
    37. 2012
  37. Vogel,R.A.
    PCSK9 inhibition: the next statin?
    J Am Coll Cardiol59, 2354-2355. PubMed  Europe PubMed DOI  T  I
    38. 2011
  38. Duff,C.J. and Hooper,N.M.
    PCSK9: an emerging target for treatment of hypercholesterolemia
    Expert Opin Ther Targets15, 157-168. PubMed  Europe PubMed DOI  T  I
  39. Tibolla,G., Norata,G.D., Artali,R., Meneghetti,F. and Catapano,A.L.
    Proprotein convertase subtilisin/kexin type 9 (PCSK9): from structure-function relation to therapeutic inhibition
    Nutr Metab Cardiovasc Dis21, 835-843. PubMed  Europe PubMed DOI  V  I

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